The present invention provides novel benzothiophene and benzofuran compounds, novel methods for synthesis thereof, selected novel intermediates, pharmaceutical compositions, and uses of the novel compounds particularly as antiallergic agents. Additionally, the compounds prevent the release of mediators including histamine and leukotrienes from basophils and mast cells, and prevent respiratory burst in neutophils providing activity useful in cardiovascular disorders as well as in antiinflammatory, psoriasis, and antimigraine treatment. These compounds act as inhibitors of cell activation. See B. Samuelsson, "Leukotrienes' Mediators of Immediate Hypersensitivity Reactions and Inflammation," Science, Vol. 220, p 568 (1983), P. J. Piper, "Leukotrienes," Trends in Pharmacological Sciences, pp 75 & 77 (1983), and J. L. Romson, et al; "Reduction of the Extent of Ischemic Myocardial Injury by Neutrophil Depletion in the Dog," Circulation, Vol. 67, p 1016 (1983)
European patent application No. (EP) 0146243 discloses a series of benzofuran and benzothiophene compounds. However, the benzothiophenes of the present invention are not included in EP No. 014623 and the benzofurans of the present invention cannot be made by the processes disclosed in EP No. 0146243.
European patent publication No. 69,521 discloses benzothiophene derivatives. However, the novel compounds of the present invention include differences, for example, having tetrazole and carboxamide substitutents, from the compounds in EP No. 069,521 not suggested by its disclosure. Additionally, U.S. Pat. No. 3,452,039 discloses benzothiophene derivatives, however, the substitutents of the present compounds are not shown.
Furthermore, the antiallergic utility now found for novel compounds of the present invention is not within the teachings for the benzothiophene compounds disclosed by either the EP No. 69,521 reference or the U.S. Pat. No. 3,452,039.